专利号:US-7034154-B2 优先权日:1999-08-10 标 题:Synthesis of substituted pyrazolopyrimidines 发明人:GROSS RAYMOND S; WILCOXEN KEITH M; OGLESBY RICHARD CHRISTOPHER 权利人:NEUROCRINE BIOSCIENCES INC 摘要:Methods of making substituted pyrazolopyrimidines generally and, more particularly, N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-α]-pyrimidin-7-yl}phenyl)acetamide. Such compounds have utility over a wide range of indications, including treatment of insomnia. In the practice of the present invention, improved techniques which do not require use and/or isolation of the pyrazole intermediate are disclosed, as well as improved techniques for making the reaction intermediates themselves. Such techniques offer significant advantages, including enhanced efficiency, particularly in the context of large scale manufacture.
专利号:US-7498434-B2 优先权日:2004-01-14 标题:Two-phase method for the synthesis of selected pyrazolopyrimidines 发明人:CANTRELL GARY LEE; MOSER FRANK WILLIAM; HALVACHS ROBERT EDWARD 权利人:MALLINCKRODT INC 摘要:An improved method of making a substituted pyrazolopyrimidine. The method comprises reacting a aminopyrazole compound or a salt thereof with a substituted 1-oxo-2-propenyl-arene(-heterocycle) or a salt thereof under acidic conditions in a reaction medium including a two-phase mixture of an aqueous solution and a water-immiscible organic liquid. Specific substituted pyrazolopyrimidines include N-[3-(3-cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide and N-methyl-N-(3-{3-[2-thienyl-carbonyl]-pyrazolo[1,5-a]-pyrimidin-7-yl}phenyl)acetamide.
专利号:WO-2004035585-A1 优先权日:2002-10-16 标 题:Synthesis of zaleplon 发明人:GURUSAMY RENUGADEVI; RAJARAM SANKARA SUBRAMANIAN 权利人:SANMAR SPECIALITY CHEMICALS LT; GURUSAMY RENUGADEVI; RAJARAM SANKARA SUBRAMANIAN 摘要:This invention relates to an improvement in the process of synthesizing N-[3-(3-cyanopyrazolo [1,5-a] pyrimindin-7-yl)phenyl]-N-ethyl acetamide. 3-dimethylamino-1-(3-N-ethyl-N-acetylaminophenyl)-2-propen-1-one is reacted with 3-aminopyrazole-4-carbonitrile in an aqueous formic acid reaction medium at a temperature ranging from 40 °C to 70 °C. This process results in better yields and higher purity of the final product.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-10226449-B2 优先权日:2013-12-20 标 题:Heterocyclic modulators of lipid synthesis and combinations thereof 发明人:HEUER TIMOTHY SEAN; OSLOB JOHAN D; MCDOWELL ROBERT S; JOHNSON RUSSELL; YANG HANBIAO; EVANCHIK MARC; ZAHARIA CRISTIANA A; CAI HAIYING; HU LILY W; DUKE GREGORY; OHOL-GUPTA YAMINI; O'FARRELL MARIE 权利人:3 V BIOSCIENCES INC 摘要:Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by dysregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
专利号:US-12291639-B2 优先权日:2017-12-14 标题:Electrically conducting poly(pyrazoles) 发明人:MARTIN BRETT D; GILES IAN D; NACIRI JAWAD; CHARLES PAUL T; TRAMMELL SCOTT A; DESCHAMPS JEFFREY R; DEPRIEST JEFFREY C 权利人:US GOV SEC NAVY 摘要:This disclosure concerns electrically conducting poly(pyrazoles). The concept of oligomerizing and polymerizing substituted aminopyrazole derivatives combined with a monomer activation procedure involving base-mediated conversion of the protonated pyrazole ring nitrogen to amine salt was developed. This disclosure concerns the specific chemistries needed for the synthesis of a pyrazole monomer used in the polymer synthesis. The procedure used for blending the novel polypyrazoles with other compounds needed for construction of solar cells for testing was developed. This disclosure concerns the concept of using these types of heteroatom-rich, electron-deficient oligomers or polymers as n-dopable or p-dopable electron acceptors in photovoltaic cells. This disclosure concerns synthesizing the starting monomer compounds and polypyrazoles.
[参考文献]: Alessandro Antonelli, Et Al. Clm29, A Multi-Target Pyrazolopyrimidine Derivative, Has Anti-Neoplastic Activity In Medullary Thyroid Cancer In Vitro And In Vivo. Mol Cell Endocrinol. 2014 Aug 5;393(1-2):56-64.
合成参考文献
摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 357. 参考文献:10.1023/b:jcam.0000004604.87558.02 摘要:Rosenfeld RJ, Goodsell DS, Musah RA, Morris GM, Goodin DB, Olson AJ. Automated docking of ligands to an artificial active site: augmenting crystallographic analysis with computer modeling. Journal of Computer-Aided Molecular Design. 2003 Aug;17(8):525–36. doi: 10.1023/b:jcam.0000004604.87558.02.